http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-063744-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_24e76490bed88751680a5fef9bc73892 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-4858 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-4866 |
| filingDate | 2007-10-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2009-02-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-063744-A1 |
| titleOfInvention | SEMISOLID FORMULATIONS OF ENZYME PHOSPHOLIPASE INHIBITORS |
| abstract | Semisolid formulations of phospholipase enzyme inhibitors, such as cytosolic PLA2, compositions containing them and processes for their manufacture. Claim 1: A pharmaceutical composition comprising a) a pharmaceutically effective amount of an active pharmacological agent having Formula (1) or its pharmaceutically acceptable salt, wherein: R is selected from the formulas - (CH2) nA, - (CH2) nSA and - (CH2) nOA, where A is selected from the portions: (2) or (3); where D is C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkyl, -CF3 or - (CH2) 1-3-CF3; B and C are independently selected from the groups phenyl pyridinyl, pyrimidinyl, furyl, thienyl and pyrrolyl, each optionally substituted with between 1 and 3 substituents independently selected from halogen, -CN, -CHO, -CF3, -OCF3, -OH, C1-6 alkyl, C1-6 alkoxy, -NH2, -N (C1-6 alkyl) 2, -NH (C1-6 alkyl), -NH-C (O) - (C1-6 alkyl), -NO2, or by a 5 or 6 membered heterocyclic or heteroaromatic ring containing 1 or 2 heteroatoms selected from O, N and S; n is an integer from 0 to 3; n1 is an integer from 1 to 3; n2 is an integer from 0 to 4; n3 is an integer from 0 to 3; n4 is an integer from 0 to 2; X1 is selected from a chemical bond, -S-, -O-, -S (O) -, -S (O) 2, - NH-, -C = C-, (4), (5) or (6 ); R1 is selected from C1-6 alkyl, fluorinated C1-6 alkyl, C3-6 cycloalkyl, tetrahydropyranyl, camphor, adamantyl, CN, -N (C1-6 alkyl) 2, phenyl, pyridinyl, pyrimidinyl, furyl, thienyl, naphthyl, morpholinyl , triazolyl, pyrazoliIo, piperidinyl, pyrrolidinyl, imidazolyl, piperizinyl, thiazolidinyl, thiomorpholinyl, tetrazolyl, indolyl, benzoxazolyl, benzofuranyl, imidazolidin-2-thionyl, 7.7, dimethyl-bicyclo [2.2.1] heptan-2-on-heptan-2-yl heptan-2-yl heptan-2-on [1,2,5] oxadiazolyl., 2-oxa-5-aza-bicyclo [2.2.1] heptanyl, piperazin-2-onyl and pyrrolyl groups, each optionally substituted with between 1 and 3 substituents independently selected from halogen, -CN, -CHO, -CF3, -OCF3 -OH, C1-6 alkyl, C1-6 alkoxy, -NH2 -N (C1-6 alkyl) 2, -NH (C1-6 alkyl), -NH-C (O ) - (C1-6 alkyl), -NO2, -SO2 (C1-3 alkyl), -SO2NH2, -SO2NH (C1-3 alkyl), -SO2N (C1-3 alkyl) 2, -COOH, -CH2-COOH, -CH2- NH (C1-6 alkyl) 2, -CH2-N (C1-6 alkyl) 2, -CH2-NH2, pyridinyl, 2-methyl-thiazolyl, morpholino, 1-chloro-2-methyl-propyl, thioalkyl-C1-6, phenyl (additionally and optionally substituted with one or more halogens, dialkylamino, -CN or -OCF3), benzyloxy, - (C1-3) alkyl (C) CH3, - (C1-3 alkyl) OCH3 , -C (O) NH2, or (7), (8), (9), (10), (11), (12) or (13); X2 is selected from -O-, -CH2-, -S-, -SO-, -SO2-, -NH-, -C (O) -, (14), (15), (16), (17) , (18), (19), or (20); R2 is an annular portion selected from phenyl, pyridinyl, pyrimidinyl, furyl, thienyl and pyrrolyl groups, the annular portion being substituted with a group of the formula - (CH2) n4-CO2H or a pharmaceutically acceptable mimetic or mimetic; and also optionally substituted with 1 or 2 additional substituents independently selected from H, halogen, -CN, -CHO, -CF3, OCF3, -OH, C1-6 alkyl, C1-6 alkoxy, C1-6 thioalkyl, -NH2, -N (C1-6 alkyl) 2, -NH (C1-6 alkyl), -NH-C (O) - (C1-6 alkyl), and -NO2; R3 is selected from H, halogen, -CN, -CHO, -CF3, -OCF3, -OH, C1-6 alkyl, C1-6 alkoxy, C1-6 thioalkyl, -NH2, -N (C1-6 alkyl) 2, -NH (C1-6 alkyl), -NH-C (O) - (C1-6 alkyl), and -NO2; R4 is selected from H, halogen, -CN, -CHO, -CF3, -OCF3, -OH, C1-6 alkyl, C1-6 alkoxy, C1-6 thioalkyl, -NH2, -N (C1-6 alkyl) 2, -NH (C1-6 alkyl), -NH-C (O) - (C1-6 alkyl), -NO2, -NH-C (O) -N (C1-3 alkyl) 2, -NR-C (O) -NH (C1-3 alkyl), -NH-C (O) -O- (C1-3 alkyl), -SO2-C1-6 alkyl, -S-cycloalkylIoC3-6, -S-CH2-C3-cycloalkyl- 6, -SO2-C3-6 cycloalkyl, -SO2-CH2-C3-6 cycloalkyl, C3-6 cycloalkyl, -CH2-C3-6 cycloalkyl, -O-C3-6 cycloalkyl, OCH2-C3-6 cycloalkyl, phenyl, benzyl, benzyloxy, morpholino, pyrrolidino, piperidinyl, piperizinyl, furanyl, thienyl, imidazolyl, tetrazolyl, pyrazinyl, pyrazolonyl, pyrazolyl, oxazolyl and isoxazolyl, the rings of each of these R4 groups, each optionally substituted with between 1 and 3 substituents selected from the group consisting of halogen, - CN, -CHO, -CF3, -OH, C1-6 alkyl, C1-6 alkoxy, - NH2, -N (C1-6 alkyl) 2, -NH (C1-6 alkyl ), -NH-C (0) - (C1-6 alkyl), -NO2, - SO2 (C1-3 alkyl), -SO2NH (C1-3 alkyl), -SO2N (al C1-3) 2, and -OCF3; each R5 is independently H or C1-3 alkyl; and R6 is H or C1-6 alkyl; and b) a carrier or excipient system comprising: i) about 15 to about 25% of a viscosity improver of the composition; ii) about 5 to about 15% of a solubilizer by weight of the composition; and iii) about 10 to about 5% of a diluent by weight of the composition; and iv) about 1 to about 1% of a stabilizer by weight of the composition. Claim 16: The pharmaceutical composition according to claim 14, wherein the compound of Formula II is 4- (3- {5-chloro-1- (diphenylmethyl) -2- [2 - ({[2- (trifluoromethyl) acid ) benzyl] sulonyl} amino) ethyl] -1H-indol-3-yl} propyl) benzoic or its pharmaceutically acceptable salt. Claim 36: A pharmaceutical composition comprising: a) an active pharmacological agent comprising 4- (3- {5-chloro-1- (diphenylmethyl) -2- [2 - ({[2 (trifluoromethyl) benzyl] sulfonyl acid) } amino) ethyl] -1H-indole-3-yl} propyl) benzoic or its pharmaceutically acceptable salt, in an amount of about 20% by weight of the composition; and b) a carrier or excipient system comprising: i) PEG 1000 in an amount of approximately 20% weight of the composition; ii) polysorbate 80 in an amount of about 10% by weight of the composition; iii) PEG 400 in an amount of approximately 40% by weight of the composition; and iv) PVP K-17 in an amount of approximately 10% by weight of the composition. |
| priorityDate | 2006-10-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 60.